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. 2021 Sep 23;240:1–8. doi: 10.1016/j.imlet.2021.09.005

Table 1.

FDA approved inhibitors of the PI3K/Akt/mTOR pathway [64, 65].

Drug Target Indication approved for (FDA) Adverse reactions
Rapamycin (Sirolimus, AY 22989 I 2190A, NSC 226080, RAPA. Rapammune…etc.) mTOR
  • -

    Renal transplant patients (prophylaxis of organ rejection).

  • -

    Lymphangioleiomyomatosis.
  • -

    Oedema

  • -

    Hypertension

  • -

    Hypertriglyceridemia

  • -

    hypercholesterolaemia

  • -

    Increased creatinine

  • -

    Abdominal pain

  • -

    Diarrhoea

  • -

    Nausea

  • -

    Headache

  • -

    Dizziness

  • -

    Fever

  • -

    Urinary tract infection

  • -

    Upper respiratory tract infection

  • -

    Nasopharyngitis

  • -

    Stomatitis

  • -

    Acne

  • -

    Anaemia

  • -

    Thrombocytopenia

  • -

    Arthralgia

  • -

    Myalgia

  • -

    Chest pain
Everolimus
(001, RAD,
40-O-(2-hydroxyethyl)-rapamycin, Afinitor,
Certican…etc		 mTOR
  • -

    Postmenopausal women with advanced hormone receptor-positive, HER2-negative breast cancer (in combination with exemestane).

  • -

    Adults with progressive neuroendocrine tumours of pancreatic origin (unresectable, locally advanced or metastatic disease).

  • -

    Adults with advanced renal cell carcinoma.

  • -

    Adults with renal angiomyolipoma and tuberous sclerosis complex

  • -

    (not requiring immediate surgery).

  • -

    Patients with tuberous sclerosis complex for treating subependymal giant cell astrocytoma (cannot be curatively resected).
  • -

    Stomatitis

  • -

    Oedema

  • -

    Rash

  • -

    Fatigue

  • -

    Headache

  • -

    Diarrhoea

  • -

    Abdominal pain

  • -

    Nausea

  • -

    Decreased appetite

  • -

    Fever

  • -

    Pyrexia

  • -

    Asthenia

  • -

    Cough

  • -

    Infections

  • -

    Upper respiratory tract infection

  • -

    Sinusitis

  • -

    Otitis media
Idelalisib (870281-82-6, CAL-101, Zydelig, GS-1101) PI3K-δ
  • -

    Relapsed Chronic lymphocytic leukaemia (in combination with rituximab)

  • -

    Relapsed follicular B-cell non-Hodgkin lymphoma

  • -

    Relapsed small lymphocytic lymphoma.
  • -

    Diarrhoea

  • -

    Nausea

  • -

    Abdominal pain

  • -

    Pyrexia

  • -

    Chills

  • -

    Fatigue

  • -

    Cough

  • -

    Pneumonia

  • -

    Rash
Copanlisib (1032568-63-0, BAY 80–6946, Aliqopa,
BAY-80-6946)		 Pan PI3K
  • -

    Adults with relapsed follicular lymphoma
  • -

    Hyperglycaemia

  • -

    Diarrhoea

  • -

    Nausea

  • -

    Decreased general strength and energy

  • -

    Hypertension

  • -

    Thrombocytopenia

  • -

    Leukopenia

  • -

    Neutropenia

  • -

    Lower respiratory tract infections
Duvelisib (COPIKTRA, 1201438-56-3, IPI-145, (S)-3-(1-((9H-Purin-6-yl)amino)ethyl)-8-chloro-2-phenylisoquinolin-1(2H)-one, INK-1197) PI3K-δ and PI3K-γ
  • -

    Adults with relapsed or refractory chronic lymphocytic leukaemia

  • -

    Adults with relapsed or refractory small lymphocytic lymphoma

  • -

    Adults with relapsed or refractory follicular lymphoma
  • -

    Diarrhoea or colitis

  • -

    Nausea

  • -

    Neutropenia

  • -

    Anaemia

  • -

    Rash

  • -

    Fatigue

  • -

    Musculoskeletal pain Pyrexia

  • -

    Cough

  • -

    Upper respiratory infection

  • -

    Pneumonia
Alpelisib (1217486-61-7, BYL-719, NVP-BYL719) PI3K-α
  • -

    Women (postmenopausal), and men, with advanced or metastatic hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative, and PIK3CA­ mutate breast cancer (in combination with fulvestrant).
  • -

    Increased/ decreased glucose

  • -

    Increased creatinine

  • -

    Diarrhoea

  • -

    Nausea

  • -

    Vomiting

  • -

    Rash

  • -

    Lymphopenia

  • -

    Anaemia

  • -

    Increased gamma glutamyl transferase increased

  • -

    Increased alanine aminotransferase

  • -

    Fatigue

  • -

    Increased lipase

  • -

    Anorexia

  • -

    Stomatitis

  • -

    Weight loss

  • -

    Decreased calcium

  • -

    Activated partial thromboplastin time prolonged

  • -

    Alopecia
Umbralisib (UKONIQ, rp-5264,
1532533-67-7, TGR-1202)		 PI3K-δ
  • -

    Relapsed or refractory marginal zone lymphoma.

  • -

    Relapsed or refractory follicular lymphoma.
  • -

    Increased creatinine

  • -

    Diarrhoea-colitis

  • -

    Nausea

  • -

    Vomiting

  • -

    Abdominal pain

  • -

    Neutropenia

  • -

    Transaminase elevation

  • -

    Anaemia

  • -

    Thrombocytopenia

  • -

    Upper respiratory tract infection

  • -

    Anorexia

  • -

    Fatigue

  • -

    Musculoskeletal pain

  • -

    Rash